Identification and characterization of 4-aryl-3,4-dihydropyrimidin-2(1H)-ones as inhibitors of the fatty acid transporter FATP4

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3504-9. doi: 10.1016/j.bmcl.2006.03.102. Epub 2006 Apr 27.

Abstract

Several potent, cell permeable 4-aryl-dihydropyrimidinones have been identified as inhibitors of FATP4. Lipophilic ester substituents at the 5-position and substitution at the para-position (optimal groups being -NO(2) and CF(3)) of the 4-aryl group led to active compounds. In two cases racemates were resolved and the S enantiomers shown to have higher potencies.

MeSH terms

  • Cell Line
  • Fatty Acid Transport Proteins / antagonists & inhibitors*
  • Humans
  • Molecular Structure
  • Pyrimidinones / chemical synthesis
  • Pyrimidinones / chemistry*
  • Pyrimidinones / pharmacology*
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Fatty Acid Transport Proteins
  • Pyrimidinones
  • SLC27A4 protein, human